| Synthesis and anti-HBV evaluation of mono L-amino acid ester,mono non-steroid anti-inflammation drug carboxylic ester derivatives of acyclonucleoside phosphonates简 |
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| 基金项目： | This work was supported by the National Natural Science Foundation of China (Nos. 20962004, 81260473), Projects of Guizhou Science and Technology Department (Nos. 2013-3031, 2012-3013), and Excellent Youth Scientific Talents Foundation of Guizhou (No. 2013-45). |
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| 摘 要： | A series of mono L-amino acid ester, mono non-steroid anti-inflammation drug(NSAID), carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a ‘‘one pot synthesis' ' method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index(SI) values of 0.48 mmol/L and 763.72, respectively.
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| 关 键 词： | L-氨基酸酯 一锅合成法 抗HBV 单声道 衍生物 羧酸酯 类固醇 膦酸盐 |
| 收稿时间： | 2013-06-16 |
| 修稿时间： | 2013-09-02 |
Synthesis and anti-HBV evaluation of mono L-amino acid ester,mono non-steroid anti-inflammation drug carboxylic ester derivatives of acyclonucleoside phosphonates |
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| Authors: | Xiao-Zhong Fu Feng-Jie Jiang Yu Ou Sheng Fu Yu-Feng Cha Shun Zhang Zong-Yuan Liu Wen Zhou Ai-Min Wanga Yong-Lin Wang |
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| Institution: | a School of Pharmacy, Guiyang Medical College, Engineering Research Center for the Development and Application of Ethnic Medicines and TCM; Ministry of Education, Guiyang 550004, China;
b Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guiyang 550004, China;
c Guiyang Women and Children's Hospital and Health Institute, Guiyang 550001, China |
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| Abstract: | A series ofmono L-amino acid ester, mono non-steroid anti-inflammation drug (NSAID), carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a "one pot synthesis" method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index (SI) values of 0.48 μmol/L and 763.72, respectively. |
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| Keywords: | Acyclonucleoside phosphonate Non-steroid anti-inflammation drug Anti-HBV activity |
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